| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| ln Vitro |
Samelisant has very high selectivity for H3R and inverse agonist action. Following administration of 1, 10, and 100 nM Samelisant, the histamine pEC50 value (8.5) of the human H3 receptor increased to 8.2, 7.3, and 6.2, respectively. Rat H3 receptors' histamine pEC50 value (8.2) rose to 7.9, 7.4, and 6.4 following treatment with 1, 10, and 100 nmol/L Samelisant, respectively [1]. Samelisant exhibits reversible binding to the positive site; Kb values of 1.3 nM and 1.1 nM, respectively, are inferred from the pA2 values of human and rat H3R [1]. Samelisant has no effect on dopamine levels in the striatum or nucleus accumbens, but it does modify dopamine and norepinephrine levels in the cerebral cortex [1].
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| ln Vivo |
Samelisant (10 and 30 mg/kg, orally administered) dramatically increased wakefulness while decreasing non-rapid eye movement (NREM) sleep in orexin deficient mice undergoing sleep electroencephalography (EEG) [1]. Moreover, samelisant dramatically delays the beginning of direct rapid eye movement (REM) sleep episodes (DREM), proving its anticonvulsant properties in narcolepsy-related animal models [1]. When mice are given Samelisant, their levels of farmethylhistamine rise in a dose-dependent manner, suggesting that histaminergic neurotransmission has been activated [1].
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| Animal Protocol |
Animal/Disease Models: Male Wistar rat or male C57BL6J mouse [1]
Doses: 1, 3, 10 and 30 mg/kg Route of Administration: Oral Experimental Results: Dose producing t-MH levels in frontal cortex, hypothalamus and hypothalamus Dependently increases cerebrospinal fluid (CSF) in male Wistar rats. Dramatically increased t-MH levels in the frontal cortex, striatum and hypothalamus of mice. |
| References |
[1]. Ramakrishna Nirogi, et al. Samelisant (SUVN-G3031), a potent, selective and orally active histamine H3 receptor inverse agonist for the potential treatment of narcolepsy: pharmacological and neurochemical characterisation. Psychopharmacology (Berl). 2021
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| Molecular Formula |
C21H33CL2N3O3
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|---|---|
| Molecular Weight |
446.411023855209
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| Elemental Analysis |
C, 56.50; H, 7.45; Cl, 15.88; N, 9.41; O, 10.75
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| CAS # |
1394808-20-8
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| Related CAS # |
Samelisant free base;1394808-82-2
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| SMILES |
Cl.Cl.O(C1C=CC(=CC=1)NC(CN1CCOCC1)=O)C1CCN(CC1)C1CCC1
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| Synonyms |
SUVN-G3031; SUVN G3031; SUVN-G 3031.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~140.01 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.66 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.66 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.66 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2401 mL | 11.2005 mL | 22.4009 mL | |
| 5 mM | 0.4480 mL | 2.2401 mL | 4.4802 mL | |
| 10 mM | 0.2240 mL | 1.1200 mL | 2.2401 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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